Insecticide and acaricide paints that inhibit chitin synthesis, regulate insect juvenile hormone and repel arthropods, for controlling endemic diseases, pests and allergens

ABSTRACT

The present invention relates to insecticide and acaricide paints that inhibit chitin synthesis, regulate insect juvenile hormone and repel arthropods, for controlling endemic diseases, pests and allergens. The paints comprise at least the following compounds (in any combination): 1%-100% water, 0.0001%-20% insecticides, 0.0001%-20% chitin inhibitor, 0.0001%-20% juvenile hormone regulator, 1%-50% polymers, 0%-40% pigments, 0%-60% fillers, 0%-60% natural repellents, and 0.01%-20% stabilizers. The composition of the paints allows the active ingredients to be encapsulated in an aqueous polymer with or without the incorporation of fillers and pigments, and therefore the range of use thereof is increased.

This application is a Continuation of International Application No.PCT/ES2009/070439.

FIELD OF THE ART

The invention refers to the field of paints, specifically to paints withinsecticide and acaricide properties for controlling endemic diseases,pests and allergens.

STATE OF THE ART

It is known the existence in the market of paints with insecticideaction (EP 871011308-2; FR 8601516; US 010300, CA 528968). However,these inventions have several significant drawbacks for the common usethereof:

-   -   they contain obsolete active principles, which are not of the        new generation,    -   some of these active principles are currently prohibited in the        European Union (e.g. organochlorine) because of their toxicity,    -   active principles, as the traditional pyrethroids, which do not        produce a residual character and have little effectiveness over        time are used.

Application GB2142239 describes the use of insecticides in a formulationfor paints and application US2006029630 describes the use of naturalrepellents for insects and arachnids in paints.

To solve these drawbacks new paints have been designed later, as thosedescribed in the Spanish patent ES2127120 for arthropods control. Saidnon-toxic and with residual character paints act as chitin synthesisinhibitors, one of the main components of the exoskeleton of arthropods.The composition of this type of paints comprises basically resin,pigment, fillers and active principles that are microencapsulated withthe polymer of the resin itself in the manufacturing process.

On the basis of these considerations, the present invention, that alsorelates to insecticide and acaricide paints, entails a step forwardagainst the state of the art given that it improves and broadens thearthropods control action claimed in the Spanish application no.2127120.

The paints disclosed herein have novel variations in the composition,both in regards to the content by weight of the compounds used in themanufacture thereof and the incorporation of a) new active principles orinsecticides, and b) new arthropod growth regulators that actcontrolling the juvenile hormone of the insects. In addition, these newpaints have a repellent action of arthropods not described in the paintsknown until now, which allows their use in places where the use ofproducts that incorporate insecticides or growth regulators of insectsis prohibited.

BRIEF DESCRIPTION OF THE INVENTION

The present invention relates to insecticide and acaricide paints, thatinhibit chitin synthesis, regulate insect juvenile hormone and repelarthropods, for controlling endemic diseases, pests and arthropods thatact as allergens.

This invention relates to a new improved and expanded formula forcontrolling all kinds of arthropods (insects, mites). This controloccurs both at the chemical level, as the formulation includes synthesisinsecticides (pyrethroids, carbamates, neonicotinoids andphenylpyrazoles, in addition to organophosphates), and at the biologicallevel, due to the incorporation of insect growth regulators (juvenilehormone analogues and chitin synthesis inhibitors).

In addition, a new active ingredient in the form of arthropod naturalrepellent is included which allows keeping them at a distance from theplaces where the formulation is applied; thus a repellent effect isachieved conferring new properties to the formulation and expanding theapplication possibilities of the formulation.

The composition of the paints allows the encapsulation of the activeingredients (insecticides, growth regulators and repellents) in anaqueous polymer with or without the addition of fillers and pigments inthe same, which increases its range of use, so that they can be appliedas conventional paints on walls and other rigid surfaces, or on othermedia that have already been scientifically tested as it is the case offabrics.

The components involved in the technology of the paints described areessentially: a) copolymers of different types, such as VeoVa-typevinylic, acrylic, and in general polymers in aqueous base; b) activeprinciples, such as insecticides, insect growth regulators and naturalrepellents; and c) the partial addition of fillers of the type ofcalcium carbonate and pigments with high luminosity and high chemicalresistance, to be used as paint. It can also be provided only with thecopolymer, without pigments or fillers, for its use as transparentemulsion.

DETAILED DESCRIPTION OF THE INVENTION

The insecticide and acaricide paints object of the present inventionhave been designed to control all kinds of arthropods due to theircapacity to inhibit the chitin synthesis, regulate the insect juvenilehormone and repel arthropods. These insecticide and acaricide paints arecharacterized in that they comprise at least the following compounds:

From To (in any combination) Water 1% 100%  Insecticides 0.0001%    20%Chitin inhibitor 0.0001%    20% Juvenile hormone 0.0001%    20%regulator Polymers 1% 50% Pigments 0% 40% Fillers 0% 60% Naturalrepellents 0% 60% Stabilizers 0.01%   20%

wherein all the percentages are by weight with respect to the totalweight of the composition, and they can be combined in any possiblevariation within the established ranges.

In a preferred embodiment, the composition of the paints is thefollowing:

% by weight of the total Insecticides  5% Chitin inhibitor 0.063%  Juvenile hormone 0.063%   regulator Polymers 14% Pigments 10% Fillers30% Natural repellents  5% Stabilizers  1% Water remaining %

The insecticides used are synthesis actives specifically created for theformulation of insecticides for use in Public Health, Animal Health andPlant Health. Preferably, said insecticides are selected from a groupconsisting of organophosphates, carbamates, pyrethroids, neonicotinoidsand phenylpyrazoles, or a combination thereof.

The action of organophosphate and carbamate is based on inhibiting theaction of the enzyme acetylcholinesterase which is responsible for nervetransmission. In turn, pyrethroids also affect the nervous system of theinsect, but acting as dissociative of the axonal membrane, keeping openthe sodium channels of said membrane. Neonicotinoids act on the centralnervous system of the insects, causing an irreversible blockade of thepostsynaptic nicotinergic acetylcholine receptors. Besides,phenylpyrazoles block the chlorine channels regulated by they-aminobutiric acid (GABA) in the neurons of the insects.

These groups have insecticides which act by contact, ingestion andinhalation and they do it on the different development stages of insectsand arachnids, although the egg stage is especially resistant to theiraction.

Preferably, organophosphate insecticides are selected from a groupconsisting of Diazinon, chlorpyrifos, methylchlorpyrifos, malathion,trichlorfon, dimethoate, dichlorvos, methamidophos, acetate, parathion,fenitrothion, fenthion and azinphos-methyl, or a combination thereof.Also preferably carbamates are selected from a group consisting ofmethomyl, aldicarb, oxamyl, thiodicarb, methiocarb, propoxur,bendiocarb, carbosulfan, fenoxycarb, pirimicarb, indoxacarb, alanycarband furathiocarb, or a combination thereof. In turn, pyrethroids arepreferably selected from a group consisting of allethrin, d-allethrin,alpha-cypermethrin, cypermethrin, permethrin, tetramethrin,bioallethrin, fenvalerate, bifenthrin, cyfluthrin, deltamethrin,prallethrin, acenathrin, imiprothrin, lambda-cyhalothrin,gamma-cyhalothrin and etofenprox, or a combination thereof. In anotherpreferred embodiment, neonicotinoids are selected from a groupconsisting of imidacloprid, acetamiprid, thiamethoxam, nitenpyram,clothianidin, dinotefuran and thiacloprid, or a combination thereof.Phenylpyrazoles are selected from fipronil and endosulfan, or acombination thereof, preferably.

The chitin synthesis inhibitors are framed within the so-called growthregulator insecticides (IGRs), and are preferably selected from a groupconsisting of flufenoxuron, hexythiazox, diflubenzuron, hexaflumuron andtriflumuron, or a combination thereof.

These inhibitors have the following way of action: the insects arecoated by a rigid exoskeleton, the integument, which provides themprotection and prevents the loss of water, allowing their survival.Insects, in order to be able to develop and due to the rigidity of theaforementioned integument, must grow in a discontinuous way. For this,they periodically get rid of the integument and create a larger new one.This process is known as “molting”.

The application of the chitin synthesis inhibitors used in the paintgives rise to a process capable of inhibiting the chitin productionmechanism, the main component of the integument. By preventing itsproduction, the formation of a new integument is blocked and as a resultthe molting process does not take place, whereby its development and,therefore, its existence is unviable.

The activity of the product affects all the stages of sensitive insectsalthough in a different way. It affects eggs of some species when theyare deposited on the vegetable parts of treated plants or when the sameare treated once deposited. Eggs can develop, but the larvae from thesame are unable to emerge or die shortly thereafter. It affects thelarval stages by preventing the molting, which leads to the appearanceof symptoms such as: double cephalic capsule, ballooning of the thorax,and displaced or deformed jaws. As a result of the inability to molt,the larvae die since they are not able to evolve to subsequent stages.Due to the aforementioned deformations, they are unable to feed, whatmakes their survival impossible. The larvae exposed to sub lethal dosesof the product can “pupate” but they do not produce viable adults orgive rise to adults who lay fewer eggs than normal. It affects theadults by reducing their fertility.

As for the juvenile hormone analogues, they are selected preferably froma group consisting of pyriproxyfen, fenoxycarb, hydroprene andmethoprene, or a combination thereof. This type of compounds acts bymaintaining high the levels of juvenile hormone (JH) in the insect. Themolting process in the insects is controlled by two hormones: β-ecdysoneand juvenile hormone. The normal development of the insect depends on aprecise adjustment of the JH concentrations at each stage. A disturbancein the relationship between the JH concentration and the developmentstage leads to abnormal development. When the JH levels are lower thanthose of β-ecdysone the molting process begins.

To prevent the maturation of the insects, the juvenile hormone and itssynthetic analogues are non-toxic and environmentally sensitive means tofight the insects which are very difficult to develop resistance. The JHanalogues do not reduce the population immediately as classicinsecticides do, but control is achieved in approximately onegeneration.

The natural insects repellents used in the manufacture of the paints areselected preferably from a group consisting of citronella, lavender oil,garlic extract, eucalyptus oils, thyme oils, basil and others extractedfrom plants with insect repellent properties, or a combination thereof.

Natural insects repellents were one of the first strategies for fightingor preventing the presence of insects within homes. Initially leaves andflowers of plants were used, then essential oils were extracted fromthese plants and, later, these oils were included in fuels, as wax andpetroleum, to release the repellent substances to the environment.

Synthesis insecticides, insect growth regulators and natural insectsrepellents are incorporated into the formulation by themicro-encapsulation process of a polymer which is detailed below.

The structure of the microcapsule is an active core and a frame thatsurrounds the first. The production process is complex, since the activesubstances (the insecticides, the insect growth regulators and theinsects repellents) are introduced in the polymer nature matrix or wallsystem, achieving, due to the polymer, a gradual release of the activeagents, inserted depending on the specific application needs of thesubstrate on which the microcapsules are deposited. The microcapsuleformation is a chemical process, both with the copolymers and theactives mixture jointly, and the micro-encapsulation of the polymerswith the juvenile growth hormone regulators, the chitin synthesisinhibitors or the repellents, all of them together or separately in thepolymer matrix in the encapsulation, resulting in a suspension ofmicrocapsules ranging between one and several hundred micrometers. Theprogressive and controlled release of the microencapsulated actives isachieved due to the nature of the polymer coating them. It has an easy,durable, resistant to rain and effective application.

With regard to the other elements that make up the paints object of thepresent invention, the resins used are preferably polymers in aqueousbase, and more preferably vinyl or acrylic copolymers or a combinationthereof. Preferably, vinyl copolymers are of the VeoVa type.

The fillers of the paints are preferably selected from a groupconsisting of calcium and magnesium carbonates, or a combination ofboth. The pigments are preferably of the titanium dioxide type. Thecomposition included in the patent allows the use or not of fillers andpigments which greatly diversifies its range of application; as it canbe applied as a conventional paint with brush, roller or “air-less”-typespray gun on walls and other rigid surfaces or, in the case of notincluding fillers or pigments in the formulation it can be applied byspraying on other supports as it is the case of all kinds offabrics—canvas, curtains, carpets, rugs, clothes.

Finally, the stabilizers used are those common in a plastic paint, beingpreferably selected from a group consisting of sodium benzoate, sodiumhexametaphosphate and sodium nitrite, or a combination thereof, amongothers. In short, the present invention provides a new methodology forcontrolling arthropods-pests, wherein a high efficiency over a widerange of arthropods as cockroaches, mosquitoes, flies, bugs, scorpions,mites and spiders is achieved through a single application. Theformulation acts primarily by contact, but it also does it byinhalation.

DESCRIPTION OF THE FIGURE

FIG. 1. Image of the structure of the microcapsule. The structure of themicrocapsule consists of an active core surrounded by a frame. Theproduction process is complex, since the active substances (theinsecticides, the insect growth regulators and the insects repellents)are introduced in the polymer nature matrix or wall system, achieving,due to the polymer, a gradual release of the active agents, inserteddepending on the specific application needs of the substrate on whichthe microcapsules are deposited.

1. Insecticide and acaricide paints, inhibitors of chitin synthesis,regulators of the juvenile hormone of insects and arthropods repellent,for controlling endemic diseases, pests and arthropods acting asallergens, characterized in that they comprise at least the followingcompounds: water, in a percentage comprised between 1% and 100%,including both limits, insecticides, in a percentage comprised between0.0001% and 20%, including both limits, chitin inhibitor, in apercentage comprised between 0.0001% and 20%, including both limits,juvenile hormone analogues, in a percentage comprised between 0.0001%and 20%, including both limits, polymers, in a percentage comprisedbetween 1% and 50%, including both limits, pigments, in a percentagecomprised between 0% and 40%, including both limits, fillers, in apercentage comprised between 0% and 60%, including both limits, naturalrepellents in a percentage comprised between 0% and 60%, including bothlimits, and stabilizers, in a percentage comprised between 0.01% and20%, including both limits, wherein all the percentages are by weightwith respect to the total weight of the composition, and they can becombined in any possible variation with the established ranges, andwherein the insecticides, the chitin inhibitor, the juvenile hormoneanalogues and the natural repellents are microencapsulated.
 2. Paintsaccording to claim 1, characterized in that they comprise the followingcomposition: insecticides: 5%, chitin inhibitor: 0.063%, juvenilehormone regulator: 0.063%, polymers: 14%, pigments: 10%, fillers: 30%,natural repellents: 5%, stabilizers: 1% and, water: remainingpercentage, wherein all the percentages are by weight with respect tothe total weight of the composition.
 3. Paints according to claim 1,wherein the insecticides are selected from a group consisting oforganophosphates, carbamates, pyrethroids, neonicotinoids andphenylpyrazoles, or a combination thereof.
 4. Paints according to claim3, wherein the organophosphates are selected from a group consisting ofDiazinon, chlorpyrifos, methylchlorpyrifos, malathion, trichlorfon,dimethoate, dichlorvos, methamidophos, acetate, parathion, fenitrothion,fenthion and azinphos-methyl, or a combination thereof.
 5. Paintsaccording to claim 3, wherein the carbamates are selected from a groupconsisting of methomyl, aldicarb, oxamyl, thiodicarb, methiocarb,propoxur, bendiocarb, carbosulfan, fenoxycarb, pirimicarb, indoxacarb,alanycarb and furathiocarb, or a combination thereof.
 6. Paintsaccording to claim 3, wherein the pyrethroids are selected from a groupconsisting of allethrin, d-allethrin, alpha-cypermethrin, cypermethrin,permethrin, tetramethrin, bioallethrin, fenvalerate, bifenthrin,cyfluthrin, deltamethrin, prallethrin, acenathrin, imiprothrin,lambda-cyhalothrin, gamma-cyhalothrin and etofenprox, or a combinationthereof.
 7. Paints according to claim 3, wherein the neonicotinoids areselected from a group consisting of imidacloprid, acetamiprid,thiamethoxam, nitenpyram, clothianidin, dinotefuran and thiacloprid, ora combination thereof.
 8. Paints according to claim 3, wherein thephenylpyrazoles are selected from fipronil and endosulfan, or acombination thereof.
 9. Paints according to claim 1, wherein the chitinsynthesis inhibitors are selected from a group consisting offlufenoxuron, hexythiazox, diflubenzuron, hexaflumuron and triflumuron,or a combination thereof.
 10. Paints according to claim 1, wherein thejuvenile hormone analogues are preferably selected from a groupconsisting of pyriproxyfen, fenoxycarb, hydroprene and methoprene, or acombination thereof.
 11. Paints according to claim 1, wherein theinsects natural repellents are preferably selected from a groupconsisting of citronella oil, lavender oil, garlic extract, eucalyptusoils, thyme oils, basil and others extracted from plants with insectrepellent properties, or a combination thereof.
 12. Paints according toclaim 1, wherein the resins used are polymers in aqueous base. 13.Paints according to claim 12, wherein the polymers are vinyl or acryliccopolymers or a combination thereof.
 14. Paints according to claim 13,wherein the vinyl copolymers are of the VeoVa type.
 15. Paints accordingto claim 1, wherein the fillers are selected from a group consisting ofcalcium and magnesium carbonates, or a combination of both.
 16. Paintsaccording to claim 1, wherein the pigments are of the titanium dioxidetype.
 17. Paints according to claim 1, wherein the stabilizers areselected from a group consisting of sodium benzoate, sodiumhexametaphosphate and sodium nitrite, or a combination thereof, amongothers.